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Target
Receptor tyrosine-protein kinase erbB-2
Ligand
BDBM13908
Substrate
Poly(Glu,Tyr)
Meas. Tech.
ChEMBL_322346 (CHEMBL873517)
IC50
210±n/a nM
Citation
 Fink, BE; Vite, GD; Mastalerz, H; Kadow, JF; Kim, SH; Leavitt, KJ; Du, K; Crews, D; Mitt, T; Wong, TW; Hunt, JT; Vyas, DM; Tokarski, JS New dual inhibitors of EGFR and HER2 protein tyrosine kinases. Bioorg Med Chem Lett 15:4774-9 (2005) [PubMed]  Article 
Target
Name:
Receptor tyrosine-protein kinase erbB-2
Synonyms:
2.7.10.1 | C-erbB-2 | CD_antigen=CD340 | ERBB2 | ERBB2_HUMAN | ErbB-2/ErbB-3 heterodimer | FASN/HER2 | HER-2 Substrate | HER2 | MLN 19 | MLN19 | Metastatic lymph node gene 19 protein | NEU | NGL | Proto-oncogene Neu | Proto-oncogene c-ErbB-2 | Tyrosine kinase-type cell surface receptor HER2 | p185erbB2
Type:
n/a
Mol. Mass.:
137894.47
Organism:
Homo sapiens (Human)
Description:
P04626
Residue:
1255
Sequence:
MELAALCRWGLLLALLPPGAASTQVCTGTDMKLRLPASPETHLDMLRHLYQGCQVVQGNLELTYLPTNASLSFLQDIQEVQGYVLIAHNQVRQVPLQRLRIVRGTQLFEDNYALAVLDNGDPLNNTTPVTGASPGGLRELQLRSLTEILKGGVLIQRNPQLCYQDTILWKDIFHKNNQLALTLIDTNRSRACHPCSPMCKGSRCWGESSEDCQSLTRTVCAGGCARCKGPLPTDCCHEQCAAGCTGPKHSDCLACLHFNHSGICELHCPALVTYNTDTFESMPNPEGRYTFGASCVTACPYNYLSTDVGSCTLVCPLHNQEVTAEDGTQRCEKCSKPCARVCYGLGMEHLREVRAVTSANIQEFAGCKKIFGSLAFLPESFDGDPASNTAPLQPEQLQVFETLEEITGYLYISAWPDSLPDLSVFQNLQVIRGRILHNGAYSLTLQGLGISWLGLRSLRELGSGLALIHHNTHLCFVHTVPWDQLFRNPHQALLHTANRPEDECVGEGLACHQLCARGHCWGPGPTQCVNCSQFLRGQECVEECRVLQGLPREYVNARHCLPCHPECQPQNGSVTCFGPEADQCVACAHYKDPPFCVARCPSGVKPDLSYMPIWKFPDEEGACQPCPINCTHSCVDLDDKGCPAEQRASPLTSIISAVVGILLVVVLGVVFGILIKRRQQKIRKYTMRRLLQETELVEPLTPSGAMPNQAQMRILKETELRKVKVLGSGAFGTVYKGIWIPDGENVKIPVAIKVLRENTSPKANKEILDEAYVMAGVGSPYVSRLLGICLTSTVQLVTQLMPYGCLLDHVRENRGRLGSQDLLNWCMQIAKGMSYLEDVRLVHRDLAARNVLVKSPNHVKITDFGLARLLDIDETEYHADGGKVPIKWMALESILRRRFTHQSDVWSYGVTVWELMTFGAKPYDGIPAREIPDLLEKGERLPQPPICTIDVYMIMVKCWMIDSECRPRFRELVSEFSRMARDPQRFVVIQNEDLGPASPLDSTFYRSLLEDDDMGDLVDAEEYLVPQQGFFCPDPAPGAGGMVHHRHRSSSTRSGGGDLTLGLEPSEEEAPRSPLAPSEGAGSDVFDGDLGMGAAKGLQSLPTHDPSPLQRYSEDPTVPLPSETDGYVAPLTCSPQPEYVNQPDVRPQPPSPREGPLPAARPAGATLERPKTLSPGKNGVVKDVFAFGGAVENPEYLTPQGGAAPQPHPPPAFSPAFDNLYYWDQDPPERGAPPSTFKGTPTAENPEYLGLDVPV
  
Inhibitor
Name:
BDBM13908
Synonyms:
CHEMBL365606 | ethyl 4-[(1-benzyl-1H-indazol-5-yl)amino]-5-(propan-2-yl)pyrrolo[1,2-a][1,2,4]triazine-6-carboxylate | pyrrolo[2,1-f][1,2,4]triazine analog 5i
Type:
Small organic molecule
Emp. Form.:
C26H26N6O2
Mol. Mass.:
454.5236
SMILES:
CCOC(=O)c1cn2ncnc(Nc3ccc4n(Cc5ccccc5)ncc4c3)c2c1C(C)C
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Poly(Glu,Tyr)
Synonyms:
poly(E:Y) 4:1 | poly(Glu4/Tyr)
Type:
Random Polymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA